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PDB: 62 件
5CBZ
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AncMR DNA Binding Domain - (+)GRE Complex
分子名称: AncMR DNA Binding Domain, DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*CP*TP*CP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*AP*GP*AP*GP*TP*GP*TP*TP*CP*TP*G)-3'), ...
著者Hudson, W.H, Ortlund, E.A.
登録日2015-07-01
公開日2015-12-23
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space.
Proc.Natl.Acad.Sci.USA, 113, 2016
5CBX
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AncGR DNA Binding Domain - (+)GRE Complex
分子名称: AncGR DNA Binding Domain, DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*GP*AP*GP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*AP*CP*TP*CP*TP*GP*TP*TP*CP*TP*G)-3'), ...
著者Hudson, W.H, Ortlund, E.A.
登録日2015-07-01
公開日2015-12-23
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space.
Proc.Natl.Acad.Sci.USA, 113, 2016
5CBY
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BU of 5cby by Molmil
AncGR2 DNA Binding Domain - (+)GRE Complex
分子名称: AncGR2 DNA Binding Domain, DNA (5'-D(*CP*CP*AP*GP*AP*AP*CP*AP*GP*AP*GP*TP*GP*TP*TP*CP*TP*G)-3'), DNA (5'-D(*TP*CP*AP*GP*AP*AP*CP*AP*CP*TP*CP*TP*GP*TP*TP*CP*TP*G)-3'), ...
著者Hudson, W.H, Ortlund, E.A.
登録日2015-07-01
公開日2015-12-23
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (1.997 Å)
主引用文献Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space.
Proc.Natl.Acad.Sci.USA, 113, 2016
8A9G
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Binary complex of 14-3-3 zeta Glucocorticoid Receptor (GR) pT524 peptide stabilised by (R)-para chloropyrrolidone1
分子名称: 14-3-3 protein zeta/delta, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 5-[(2~{R})-3-(4-chlorophenyl)carbonyl-2-(4-nitrophenyl)-4-oxidanyl-5-oxidanylidene-2~{H}-pyrrol-1-yl]-2-oxidanyl-benzoic acid, ...
著者Munier, C.C, Edman, K, Perry, M.W.D, Ottmann, C.
登録日2022-06-28
公開日2022-12-28
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.961 Å)
主引用文献Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3-3 Protein-Protein Interaction.
J.Med.Chem., 65, 2022
8VKZ
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BU of 8vkz by Molmil
Crystal structure of Glucocorticoid Receptor in complex with an inhibitor
分子名称: (4aR,4bS,5R,6aS,6bS,8R,9aR,10aR,10bR)-8-{4-[(3-aminophenyl)methyl]phenyl}-5-hydroxy-6b-(hydroxyacetyl)-4a,6a-dimethyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H,8H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-2-one, Glucocorticoid receptor, Nuclear receptor coactivator 2
著者Judge, R.A, Hobson, A.D.
登録日2024-01-10
公開日2024-01-24
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (2.133 Å)
主引用文献Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties.
Rsc Med Chem, 15, 2024
4CSJ
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BU of 4csj by Molmil
The discovery of potent selective glucocorticoid receptor modulators, suitable for inhalation
分子名称: 1,2-ETHANEDIOL, GLUCOCORTICOID RECEPTOR, N-[(2S)-1-[[1-(4-fluorophenyl)indazol-4-yl]amino]propan-2-yl]-2,4,6-trimethyl-benzenesulfonamide, ...
著者Edman, K, Ahlgren, R, Bengtsson, M, Bladh, H, Backstrom, S, Dahmen, J, Henriksson, K, Hillertz, P, Hulikal, V, Jerre, A, Kinchin, L, Kase, C, Lepisto, M, Mile, I, Nilsson, S, Smailagic, A, Taylor, J, Tjornebo, A, Wissler, L, Hansson, T.
登録日2014-03-07
公開日2014-05-07
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献The Discovery of Potent and Selective Non-Steroidal Glucocorticoid Receptor Modulators, Suitable for Inhalation.
Bioorg.Med.Chem.Lett., 24, 2014
5UC3
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Structure of the dominant negative mutant Glucocorticoid Receptor alpha (L733K/N734P) complexed with RU-486
分子名称: (4S)-2-METHYL-2,4-PENTANEDIOL, 1,2-ETHANEDIOL, 11-(4-DIMETHYLAMINO-PHENYL)-17-HYDROXY-13-METHYL-17-PROP-1-YNYL-1,2,6,7,8,11,12,13,14,15,16,17-DODEC AHYDRO-CYCLOPENTA[A]PHENANTHREN-3-ONE, ...
著者Min, J, Cidlowski, J.A, Pedersen, L.C.
登録日2016-12-21
公開日2017-12-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.009 Å)
主引用文献Nuclear receptor
To Be Published
4LSJ
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Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Bound to a Dibenzoxapine Sulfonamide
分子名称: D30 peptide, Glucocorticoid receptor, N-{3-[(1Z)-1-(10-methoxydibenzo[b,e]oxepin-11(6H)-ylidene)propyl]phenyl}methanesulfonamide
著者Carson, M, Luz, J.G, Clawson, D, Coghlan, M.
登録日2013-07-22
公開日2014-01-29
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.35 Å)
主引用文献Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
J.Med.Chem., 57, 2014
4MDD
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BU of 4mdd by Molmil
Crystal Structure of the Glucocorticoid Receptor Bound to a Non-steroidal Antagonist Reveals Repositioning and Partial Disordering of Activation Function Helix 12
分子名称: Glucocorticoid receptor, N-[2-{[benzyl(methyl)amino]methyl}-3-(4-fluoro-2-methoxyphenyl)-5-(propan-2-yl)-1H-indol-7-yl]methanesulfonamide, Nuclear receptor corepressor 1
著者Coghlan, M.J, Luz, J.G.
登録日2013-08-22
公開日2014-12-03
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Crystal Structure of the Glucocorticoid Receptor Bound to a Non-steroidal Antagonist Reveals Repositioning and Partial Disordering of Activation Function Helix 12
To be Published
5G5W
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BU of 5g5w by Molmil
Structure guided design and discovery of Indazole ethers as highly potent, non-steroidal Glucocorticoid receptor modulators
分子名称: 1,2-ETHANEDIOL, 2,2,2-trifluoro-N-[(1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-phenylpropan-2-yl]acetamide, GLUCOCORTICOID RECEPTOR, ...
著者Hemmerling, M, Edman, K, Lepisto, M, Eriksson, A, Ivanova, S, Dahmen, J, Rehwinkel, H, Berger, M, Hendrickx, R, Dearman, M, Jellesmark-Jensen, T, Wissler, L, Hansson, T.
登録日2016-06-08
公開日2017-02-15
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Discovery of Indazole Ethers as Novel, Potent, Non-Steroidal Glucocorticoid Receptor Modulators.
Bioorg.Med.Chem.Lett., 26, 2017
5G3J
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Discovery of New Selective Glucocorticoid Receptor Agonist Leads
分子名称: 1,2-ETHANEDIOL, 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, 5-[[(1S,2R,4R)-4-ethyl-6,7-bis(fluoranyl)-2,5-bis(oxidanyl)-2-(trifluoromethyl)-3,4-dihydro-1H-naphthalen-1-yl]amino]-1H-quinolin-2-one, ...
著者Berger, M, Edman, K, Wissler, L, Neuhaus, R, Rehwinkel, H, Schacke, H, Jaroch, S.
登録日2016-04-27
公開日2017-02-15
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Discovery of New Selective Glucocorticoid Receptor Agonist Leads.
Bioorg.Med.Chem.Lett., 27, 2017
4P6X
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BU of 4p6x by Molmil
Crystal Structure of cortisol-bound glucocorticoid receptor ligand binding domain
分子名称: (11alpha,14beta)-11,17,21-trihydroxypregn-4-ene-3,20-dione, Glucocorticoid receptor, Nuclear receptor coactivator 2
著者He, Y, Zhou, X.E, Tolbert, W.D, Powell, K, Melcher, K, Xu, H.E.
登録日2014-03-25
公開日2014-04-16
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Structures and mechanism for the design of highly potent glucocorticoids.
Cell Res., 24, 2014
7KW7
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BU of 7kw7 by Molmil
Atomic cryoEM structure of Hsp90-Hsp70-Hop-GR
分子名称: ADENOSINE-5'-DIPHOSPHATE, Glucocorticoid receptor, Heat shock 70 kDa protein 1A, ...
著者Wang, R.Y, Noddings, C.M, Kirschke, E, Myasnikov, A, Johnson, J.L, Agard, D.A.
登録日2020-11-30
公開日2021-12-08
最終更新日2024-05-29
実験手法ELECTRON MICROSCOPY (3.57 Å)
主引用文献Structure of Hsp90-Hsp70-Hop-GR reveals the Hsp90 client-loading mechanism.
Nature, 601, 2022
7KRJ
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The GR-Maturation Complex: Glucocorticoid Receptor in complex with Hsp90 and co-chaperone p23
分子名称: ADENOSINE-5'-TRIPHOSPHATE, DEXAMETHASONE, Glucocorticoid receptor, ...
著者Noddings, C.M, Wang, Y.-R, Agard, D.A.
登録日2020-11-20
公開日2022-01-12
最終更新日2024-05-29
実験手法ELECTRON MICROSCOPY (2.56 Å)
主引用文献Structure of Hsp90-p23-GR reveals the Hsp90 client-remodelling mechanism.
Nature, 601, 2021
8FFW
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BU of 8ffw by Molmil
Cryo-EM structure of the GR-Hsp90-FKBP51 complex
分子名称: ADENOSINE-5'-TRIPHOSPHATE, DEXAMETHASONE, Glucocorticoid receptor, ...
著者Noddings, C.M, Agard, D.A.
登録日2022-12-10
公開日2023-11-01
最終更新日2023-12-20
実験手法ELECTRON MICROSCOPY (3.23 Å)
主引用文献Cryo-EM reveals how Hsp90 and FKBP immunophilins co-regulate the glucocorticoid receptor.
Nat.Struct.Mol.Biol., 30, 2023
8FFV
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Cryo-EM structure of the GR-Hsp90-FKBP52 complex
分子名称: ADENOSINE-5'-TRIPHOSPHATE, DEXAMETHASONE, Glucocorticoid receptor, ...
著者Noddings, C.M, Agard, D.A.
登録日2022-12-10
公開日2023-11-01
最終更新日2023-12-20
実験手法ELECTRON MICROSCOPY (3.01 Å)
主引用文献Cryo-EM reveals how Hsp90 and FKBP immunophilins co-regulate the glucocorticoid receptor.
Nat.Struct.Mol.Biol., 30, 2023
5NFP
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BU of 5nfp by Molmil
Glucocorticoid Receptor in complex with budesonide
分子名称: (1~{S},2~{S},4~{R},6~{R},8~{S},9~{S},11~{S},12~{S},13~{R})-9,13-dimethyl-11-oxidanyl-8-(2-oxidanylethanoyl)-6-propyl-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one, 1,2-ETHANEDIOL, 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, ...
著者Edman, K, Wissler, L.
登録日2017-03-15
公開日2017-10-04
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
J. Med. Chem., 60, 2017
4UDD
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BU of 4udd by Molmil
GR in complex with desisobutyrylciclesonide
分子名称: 1,2-ETHANEDIOL, 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, DESISOBUYTYRYL CICLESONIDE, ...
著者Edman, K, Hogner, A, Hussein, A, Bjursell, M, Aagaard, A, Backstrom, S, Bodin, C, Wissler, L, Jellesmark-Jensen, T, Cavallin, A, Karlsson, U, Nilsson, E, Lecina, D, Takahashi, R, Grebner, C, Lepisto, M, Guallar, V.
登録日2014-12-09
公開日2015-11-25
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献Ligand Binding Mechanism in Steroid Receptors: From Conserved Plasticity to Differential Evolutionary Constraints.
Structure, 23, 2015
4UDC
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GR in complex with dexamethasone
分子名称: 3-[(3-CHOLAMIDOPROPYL)DIMETHYLAMMONIO]-1-PROPANESULFONATE, DEXAMETHASONE, GLUCOCORTICOID RECEPTOR, ...
著者Edman, K, Hogner, A, Hussein, A, Bjursell, M, Aagaard, A, Backstrom, S, Bodin, C, Wissler, L, Jellesmark-Jensen, T, Cavallin, A, Karlsson, U, Nilsson, E, Lecina, D, Takahashi, R, Grebner, C, Lepisto, M, Guallar, V.
登録日2014-12-09
公開日2015-11-25
最終更新日2023-12-20
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Ligand Binding Mechanism in Steroid Receptors: From Conserved Plasticity to Differential Evolutionary Constraints.
Structure, 23, 2015
5NFT
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Glucocorticoid Receptor in complex with AZD5423
分子名称: 1,2-ETHANEDIOL, 2,2,2-tris(fluoranyl)-~{N}-[(1~{R},2~{S})-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]ethanamide, Glucocorticoid receptor, ...
著者Edman, K, Wissler, L.
登録日2017-03-15
公開日2017-10-04
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
J. Med. Chem., 60, 2017
4HN6
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GR DNA Binding Domain R460D/D462R - TSLP nGRE Complex
分子名称: DNA (5'-D(*AP*GP*CP*TP*CP*TP*CP*CP*CP*GP*GP*AP*GP*GP*CP*G)-3'), DNA (5'-D(*CP*GP*CP*CP*TP*CP*CP*GP*GP*GP*AP*GP*AP*GP*CP*T)-3'), Glucocorticoid receptor, ...
著者Hudson, W.H, Youn, C.E, Ortlund, E.A.
登録日2012-10-18
公開日2012-12-12
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.549 Å)
主引用文献The structural basis of direct glucocorticoid-mediated transrepression.
Nat.Struct.Mol.Biol., 20, 2013
4P6W
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Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain
分子名称: Glucocorticoid receptor, MOMETASONE FUROATE, Nuclear receptor coactivator 2
著者He, Y, Zhou, X.E, Tolbert, W.D, Powell, K, Melcher, K, Xu, H.E.
登録日2014-03-25
公開日2014-04-16
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (1.951 Å)
主引用文献Structures and mechanism for the design of highly potent glucocorticoids.
Cell Res., 24, 2014
4HN5
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BU of 4hn5 by Molmil
GR DNA Binding Domain - TSLP nGRE Complex
分子名称: DNA (5'-D(*AP*GP*CP*TP*CP*TP*CP*CP*CP*GP*GP*AP*GP*GP*CP*G)-3'), DNA (5'-D(*CP*GP*CP*CP*TP*CP*CP*GP*GP*GP*AP*GP*AP*GP*CP*T)-3'), Glucocorticoid receptor, ...
著者Hudson, W.H, Youn, C.E, Ortlund, E.A.
登録日2012-10-18
公開日2012-12-12
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (1.902 Å)
主引用文献The structural basis of direct glucocorticoid-mediated transrepression.
Nat.Struct.Mol.Biol., 20, 2013
3BQD
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BU of 3bqd by Molmil
Doubling the Size of the Glucocorticoid Receptor Ligand Binding Pocket by Deacylcortivazol
分子名称: 1-[(1R,2R,3aS,3bS,10aR,10bS,11S,12aS)-1,11-dihydroxy-2,5,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,7,10,10a,10b,11,12,12a-dodecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]-2-hydroxyethanone, Glucocorticoid receptor, Nuclear receptor coactivator 1
著者Xu, H.E.
登録日2007-12-20
公開日2008-01-15
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Doubling the size of the glucocorticoid receptor ligand binding pocket by deacylcortivazol.
Mol.Cell.Biol., 28, 2008
6EL6
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Glucocorticoid Receptor in complex with compound 4
分子名称: 1,2-ETHANEDIOL, Glucocorticoid receptor, Nuclear receptor coactivator 2, ...
著者Edman, K, Wissler, L.
登録日2017-09-28
公開日2018-02-21
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
J. Med. Chem., 61, 2018

 

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